Anticancer sustained-released gel injection and preparation method thereof

A technology for slow-release gel injections and release regulators, which is applied in the field of anti-cancer slow-release gel injections and their preparation, and in the field of slow-release gel injections. Dispersion and other issues

Inactive Publication Date: 2009-01-07
济南基福医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, in most cases, the final sustained-release formulations are mostly solid shapes (eg, microspheres, tablets, or rods), which require a more complicated implantation process and are prone to tissue trauma and even tumor cell seeding or dissemination
In addition, organi...

Method used

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  • Anticancer sustained-released gel injection and preparation method thereof
  • Anticancer sustained-released gel injection and preparation method thereof
  • Anticancer sustained-released gel injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Put 4, 2, 1 and 0.5g of amphiphilic block copolymers (PLGA-PEG-PLGA) into four containers of A, B, C and D respectively, and then pour them into four containers of A, B, C and D respectively Add 6, 8, 9 and 9.5 milliliters of water for injection into the container to prepare 40%, 20%, 10% and 5% hydrogels.

[0067] The molecular weight of polyethylene glycol in the amphiphilic block copolymer is 800-1200, accounting for 20% of the weight of the amphiphilic block copolymer; in the glycolide-lactide copolymer, the ratio of glycolide and lactide The molar ratio is 6:1.

Embodiment 2

[0069] Measure the gelation temperature of four kinds of hydrogels in embodiment 1, the result shows that the gelation temperature of 40% and 20% hydrogel is respectively 28 ℃ (40%) and 35 ℃ (20%), and 10 The gelation temperatures of the % and 5% hydrogels were not determined at 10°C-38°C.

Embodiment 3

[0071] Put 4, 2, 1 and 0.5g of amphiphilic block copolymers (PLGA-PEG-PLGA) into four containers of A, B, C and D respectively, and then pour them into four containers of A, B, C and D respectively Add 6, 8, 9 and 9.5 milliliters of water for injection into the container to prepare 40%, 20%, 10% and 5% hydrogels.

[0072] The molecular weight of polyethylene glycol in the amphiphilic block copolymer is 1200-1600, accounting for 15% of the weight of the amphiphilic block copolymer; in the glycolide-lactide copolymer, the ratio of glycolide and lactide The molar ratio is 4:1.

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Abstract

The invention relates to an anticancer slow-release gel injection and a preparation method thereof. The anticancer slow-release gel injection contains a taxane-like drug such as paclitaxel, docetaxel, hydroxypaclitaxel, epi-paclitaxel or deacetylpaclitaxel, a stine-like drug, an amphiphilic block polymer and a solvent. The composition exhibits the property of temperature-sensitive gelation, is a flowable liquid at the room temperature and turns into a stagnant and biodegradable water-insoluble gel in vivo in warm-blooded animals. The stine-like drug is selected from atrimustine, ambnmustine, nimustine, bendamustine, carmustine, elmustine, galamustine, fotemustine, estramustine, hesmustine, neptamustine, lomustine, semustine, ranimustine, semustine, tauromustine, tallimustine and spiromustine. The anticancer slow-release gel injection can release the drug slowly and locally around the tumor and retain the effective blood concentration for a plurality of weeks to a plurality of months, can not only kill tumor cells but also effectively inhibit tumor vessels, can reduce the general drug toxicity and can enhance the curative effect of chemotherapy particularly radioactive seed implantation.

Description

(1) Technical field [0001] The invention relates to an anti-cancer sustained-release gel injection and a preparation method thereof, belonging to the technical field of medicines. Specifically, the invention relates to a slow-release gel preparation capable of stably releasing taxanes and statins locally in solid tumors, mainly slow-release gel injections. It is an aqueous solution, which can become a semi-solid or solid gel in warm-blooded animals. (2) Background technology [0002] Although conventional chemotherapy has been used for a long time, its therapeutic effect on solid tumors is uncertain. Since the effect of chemotherapy depends on the action time and drug concentration of the drug at the tumor site, conventional chemotherapy cannot achieve the above goals. In addition, low doses of chemotherapeutic drugs can also induce drug resistance of tumor cells, and inappropriate chemotherapy can stimulate the proliferation and metastasis of tumors. [0003] Local appli...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K45/06A61K47/34A61P35/00A61K47/26A61K47/36
Inventor 孙启明孙忠先
Owner 济南基福医药科技有限公司
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